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HRID 322000作成日:2026年10月26日

Formic Acid → (+/-)-7-Chloro-1,3,4,10b-tetrahydropyrido[2,1-a]isoindole-2,6-dione

https://huagongshe.com/reaction/322000

反応式

関与物質

役割名称HCID仕込み量
反応物Formic AcidHCID 284—
反応物TriethylamineHCID 8471—
反応物1-(2-Bromo-chlorobenzoyl)-2,3-dihydro-4-pyridinoneHCID 22008820—
触媒Palladium(2+) acetate--triphenylphosphane (1/2/2)HCID 84538—
溶媒DimethylformamideHCID 6228—
生成物(+/-)-7-Chloro-1,3,4,10b-tetrahydropyrido[2,1-a]isoindole-2,6-dioneHCID 2200881931.1%

反応条件

温度80 °C

反応手順

A mixture of 1-(2-bromo-chlorobenzoyl)-2,3-dihydro-4-pyridinone (Preparation 3) (300 mg, 0.954 mmol), triethylamine (0.39 mmol, 0.54 ml), formic acid (0.05 ml, 1.3 mmol) and di(triphenylphosphine) diacetoxypalladium (47 mg, 0.063 mmol) in DMF (3 ml) was heated to 80° C. for 2 h. The cooled solution was filtered through celite, diluted with water, extracted twice with ethyl acetate, the extracts dried over sodium sulphate and evaporated. The residue was purified by flash column chromatography on silica eluting with 50% ethyl acetate in hexane to yield the title compound as a colourless oil (70 mg). MS (+CI) m/z 235/237 [M+H]+.

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US06211189B1
出典データセットuspto-grants-2001_04
ORD IDord-d095710205ce4149af120fea9605be03
出典メモuspto-grants-2001_04